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Nonshared hetero atoms in at least two rings of the polycyclo ring system

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514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514075000 - Phosphorus containing other than solely as part of an inorganic ion in an addition salt DOAI

514079000 - Nitrogen containing hetero ring

514080000 - Polycylo ring system having a ring nitrogen in the system

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DocumentTitleDate
20130045950Phosphonate Compounds - The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.02-21-2013
20120202776PHOSPHORUS DERIVATIVES AS KINASE INHIBITORS - The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.08-09-2012
20130029940PHOSPHONATES WITH REDUCED TOXICITY FOR TREATMENT OF VIRAL INFECTIONS - There are provided, inter alia, acyclic nucleoside phosphonate compounds having reduced toxicity and enhanced antiviral activity, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds for inhibiting viral RNA-dependent RNA polymerase, inhibiting viral reverse transcriptase, inhibiting replication of virus, including hepatitis C virus or a human retrovirus, and treating a subject infected with a virus, including hepatitis C virus or a human retrovirus.01-31-2013
20120184511Novel Pharmaceutical Composition Comprising a Macrolide Immunosuppressant Drug - The invention provides novel pharmaceutical compositions of macrolide immunosuppressants. The compositions comprise a hydrophilic component, a lipophilic component, and an amphiphilic component. Preferably, the compositions are formulated as liquid microemulsion. Furthermore, the invention provides uses of such compositions, such as for the topical treatment of inflammatory and autoimmune diseases. Methods for preparing the compositions are also provided.07-19-2012
20110195934AZOLOPYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable faints thereof according to08-11-2011
20120245127Methods of Treating Cell Proliferative Disorders - The present disclosure provides methods for the treatment of cell proliferative disorders by administration of a Syk kinase or Syk/Flt-3 kinase inhibitor. Cell proliferative disorders treatable by the methods include, hematopoietic neoplasms and virally associated tumors. The compounds are also directed to therapeutic or prophylactic inhibition of tumor metastasis.09-27-2012
20130035313Nucleoside Phosphonate Salts - The present invention relates to compounds and methods for treating viral diseases. Some compounds of the invention are described by Formula I: (I), wherein M02-07-2013
20090275534NOVEL PYRIDOPYRAZINE DERIVATIVES, PROCESS OF MANUFACTURING AND USES THEREOF - The invention relates to pyrido[2,3-b]pyrazine compounds of general formulae (Ia) and (Ib), to their preparation and use, for example, for the treatment of malignant disorders and other disorders based on pathological cell proliferations.11-05-2009
20130040914PRODRUGS OF AN HIV REVERSE TRANSCRIPTASE INHIBITOR - Compounds of Formula I are described: (I), wherein R02-14-2013
20120208785Prodrugs of 2,4-Pyrimidinediamine Compounds and Their Uses - The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.08-16-2012
20090156558PHOSPHONATE ANALOGS OF ANTIMETABOLITES - The invention is related to phosphorus substituted antimetabolites, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.06-18-2009
20090156557KINASE INHIBITORS - Compounds are provided for use with kinases that comprise a compound selected from the group consisting of:06-18-2009
20100093667SALTS OF HIV INHIBITOR COMPOUNDS - The invention is related to salts of anti-viral compounds, compositions containing such salts, and therapeutic methods that include the administration of such salts, as well as to processes and intermediates useful for preparing such salts.04-15-2010
20090124580PRODRUGS OF 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES - The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.05-14-2009
20130072460Methods Of Treating Retroviral Infections And Related Dosage Regimes - The present invention relates to compounds and methods for treating retroviral infections and/or Hepatitis B viral infections. Some compounds of the invention are described by Formula (I) or a stereoisomer, a diastereomer, an enantiomer or racemate thereof.03-21-2013
20130072459PHARMACEUTICAL COMPOSITION FOR THE PREVENTION OR THE TREATMENT OF NON-ALCOHOLIC FATTY LIVER DISEASE AND THE METHOD FOR PREVENTION OR TREATMENT OF NON-ALCOHOLIC FATTY LIVER DISEASE USING THE SAME - The present invention provides a pharmaceutical composition for the prevention and treatment of a non-alcoholic fatty liver disease (NAFLD), containing an active ingredient selected from the group consisting of Compound 1 represented by formula 1, sitagliptin, vildagliptin, linagliptin or a pharmaceutically acceptable salt thereof. Further, the present invention provides a method for the prevention or treatment of a non-alcoholic fatty liver disease, including administering an effective amount of an active ingredient selected from the group consisting of Compound 1 represented by formula 1, sitagliptin, vildagliptin, linagliptin or a pharmaceutically acceptable salt thereof to a mammal including a human in need thereof. Further, the present invention provides use of Compound 1 represented by formula 1, sitagliptin, vildagliptin, linagliptin or a pharmaceutically acceptable salt thereof, for manufacturing a pharmaceutical composition for the prevention or treatment of a non-alcoholic fatty liver disease.03-21-2013
20130072458Methods of Treating Viral Associated Diseases - The present invention provides methods of treating diseases associated with at least one virus. The methods include administering a compound described in the invention in a therapeutically effective amount. According to some aspects of the present invention, the methods may further comprise at least one immunosuppressant agent to treat diseases associated with at least one virus of a subject in need of immunosuppressant agents.03-21-2013
20110015155Deuterated 2, 4-Pyrimidinediamine Compounds and Prodrugs Thereof and Their Uses - The present disclosure provides biologically active deuterated 2,4-pyrimidinediamine compounds and prodrugs thereof, compositions comprising the deuterated compounds, intermediates and methods for synthesizing the deuterated compounds and methods of using the deuterated compounds in a variety of applications.01-20-2011
20130065856TENOFOVIR ALAFENAMIDE HEMIFUMARATE - A hemifumarate form of 9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine (tenofovir alafenamide), and antiviral therapy using tenofovir alafenamide hemifumarate (e.g., anti-HIV and anti-HBV therapies).03-14-2013
20090131370Novel Nucleoside Derivatives - Compounds of Formulae I-XVI, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of viral diseases including hepatitis C viral infection, cancer, diabetes, and other diseases are described: formula (I).05-21-2009
20090012045Methods of Treating Cell Proliferative Disorders - The present disclosure provides methods for the treatment of cell proliferative disorders by administration of a RET kinase inhibitor. Cell proliferative disorders treatable by the methods include, thyroid tumors.01-08-2009
20130165414PHOSPHATE ESTERS OF NORIBOGAINE - Disclosed herein are phosphate esters of noribogaine and dihydronoribogaine, and esters and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the methods of their use, including in the treatment of addiction and/or pain.06-27-2013
20120270841Diazonamide Analogs - Diazonamide analogs having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders, and related pharmaceutical compositions are provided.10-25-2012
20130165413PROCESS FOR THE PREPARATION OF TENOFOVIR - The present invention provides a process for the preparation of tenofovir. The present invention also provides a process for the preparation of tenofovir disoproxil or a salt thereof and its pharmaceutical composition using the tenofovir of the present invention.06-27-2013
20130165415CHEMICAL COMPOUNDS - The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.06-27-2013
20120309717COMPOUNDS, METHODS AND PHARMACEUTICAL COMPOSITIONS FOR INHIBITING PARP - The present invention provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.12-06-2012
20100035841INHIBITORS OF TYROSINE KINASES AND USES THEREOF - Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.02-11-2010
20110281821Modulators of Mitotic Kinases - The invention relates to compounds of Formula (I), a polymorph, an enantiomer, a stereoisomer, a solvate, an N-oxide derivative, or a pharmaceutically acceptable salt thereof: Formula (I), which have inhibitory effect on one or more protein kinases that are involved in cell mitosis.11-17-2011
20100267672NOVEL COMPOUNDS OF REVERSE-TURN MIMETICS, METHOD FOR MANUFACTURING THE SAME AND USE THEREOF - Disclosed are novel reverse turn mimetics based on the framework of pyrazino-triazinone, and the use thereof in the treatment of cancers, particularly, acute myeloid leukemia. A method is also provided for manufacturing the reverse turn mimetics on a mass scale.10-21-2010
20110301125Method for Treating Macular Degeneration - Provided herein are novel and useful methods for preventing, treating, or ameliorating a macular degeneration such as dry macular degeneration, wet macular degeneration and age related macular degeneration in a patient.12-08-2011
20110288054COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.11-24-2011
20110172192METHOD AND COMPOSITIONS FOR TREATING HEMATOLOGICAL MALIGNANCIES - A compound of formula 107-14-2011
20100004207Inhibitors of cyclin-dependent kinases, compositions and uses related thereto - The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.01-07-2010
20110201575STABILIZED SOLID DISPERSION OF ADEFOVIR DIPIVOXIL AND PREPARATION METHOD THEREOF - The present invention relates to an amorphous solid dispersion with improved stability comprising 9-[2-[[bis[(pivaloyloxy)methyl]phosphono]methoxy]ethyl]adenine as a nucleotide analogue, a pharmaceutical composition comprising the same, and a method for preparing the same.08-18-2011
20090298794HYDROXY SUBSTITUTED THIENO PYRIMIDINONES AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - The present invention provides compounds having the following Formula IA and IB, which are useful as MCHR1 antagonists, and includes prodrugs and pharmaceutically acceptable salts thereof:12-03-2009
20100120718COMBINATION THERAPY OF SUBSTITUTED OXAZOLIDINONES - The present invention relates to combinations of A) oxazolidinones of the formula (I) with B) acetylsalicylic acid (aspirin) and C) an ADP receptor antagonist, in particular P05-13-2010
20100249068SUBSTITUTED NUCLEOSIDE AND NUCLEOTIDE ANALOGS - Disclosed herein are nucleotide analogs with protected phosphates, methods of synthesizing nucleotide analogs with protected phosphates and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the nucleotide analogs with protected phosphates.09-30-2010
20100249067Modulators of Mitotic Kinases - The invention relates to compounds of Formula (I), a polymorph, an enantiomer, a stereoisomer, a solvate, an N-oxide derivative, or a pharmaceutically acceptable salt thereof: Formula (I), which have inhibitory effect on one or more protein kinases that are involved in cell mitosis.09-30-2010
20110172191THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS - A series of thieno[2,3-b]pyridine derivatives, attached at the 2-position to a substituted anilino moiety, which are substituted in the 3-position by a carbonyl group linked to a pyrrolidin-1-yl ring which in turn forms part of a heteroatom-containing fused bicyclic ring system, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.07-14-2011
20090291921INTEGRASE INHIBITORS - Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.11-26-2009
20080275004N-Substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase - N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula:11-06-2008
20080287397Pyrrolopyrimidine Derivatives Substituted with Cyclic Amino Group - An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.11-20-2008
20100292189OLIGONUCLEOTIDE ANALOG AND METHOD FOR TREATING FLAVIVIRUS INFECTIONS - A method of inhibiting replication of a flavivirus in animal cells, and an oligonucleotide compound for use in the method are disclosed. The oligonucleotide analog (i) has a nuclease-resistant backbone, (ii) is capable of uptake by the cells, (iii) contains between 8-40 nucleotide bases, and (iv) has a sequence of at least 8 bases complementary to a region of the virus' positive strand RNA genome that includes at least a portion of SEQ ID NOS:1-4. Exposure of cells infected with a flavivirus to the analog is effective to form within the cells, a heteroduplex structure composed of the virus ssRNA and the oligonucleotide, characterized by a Tm of dissociation of at least 45° C., and having disrupted base pairing between the virus' 5′ and 3′ cyclization sequences.11-18-2010
20080287398COLD MENTHOL RECEPTOR-1 ANTAGONISTS - The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.11-20-2008
20120196834Highly stable compositions of orally active nucleotide analogues or orally active nucleotide analogue prodrugs - Disclosed are highly stable compositions having outstanding storage stability and/or demonstrating exceptional resistance to aqueous solution degradation, the composition including an orally active nucleotide analogue or an orally active nucleotide analogue prodrug, which is orally bioavailable, such as adefovir dipivoxil and tenofovir disoproxil. For example, when a composition of the invention is stored for 1 month or for 18 months at 25° C. and 60% relative humidity, its orally active nucleotide analogue or orally active nucleotide analogue prodrug degrades to provide a composition containing no more than 0.2% or no more than 0.7% by weight of a less orally bioavailable impurity, respectively. Also disclosed are a container/closure package system including the composition and a package insert and methods of manufacturing the composition and treating a patient for a disease or condition, for example, a viral disease or cancer, with the use of the composition.08-02-2012
20090012046Methods of Treating Mutated Hiv - Nucleotide-competing reverse transcriptase inhibitors (NcRTI) bind to the active site of HIV reverse transcriptase (RT) in competition with the next incoming nucleotide. To further investigate the impact of RT inhibitor resistance mutations on the activity of NcRTIs, the susceptibility of >6000 recent clinical isolates for a prototype compound, NcRTI-1, was determined. Over 80% of the profiled clinical isolates remained susceptible for NcRTI-1 (FC<4). No cross-resistance was observed between NcRTI-1 and currently used RT inhibitors, apart from limited cross-resistance with 3TC/FTC.01-08-2009
20080318905Prodrugs and methods of making and using the same - Prodrugs of parent drugs and methods of making and using the same are described. The prodrugs comprise an amine-containing parent drug moiety and a prodrug moiety, such as methoxyphosphonic acid or ethoxyphosphonic acid. The prodrugs may be employed in therapy for the treatment of various indications, such as pain, and in methods of decreasing the abuse potential of abuse-prone drugs and/or delaying the onset of parent drug activity and/or prolonging parent drug activity as compared to administration of a parent drug.12-25-2008
20090325904MALEIC ACID MONOSALT OF ANTIVIRAL AGENT AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME - The present invention relates to 3-[({1-[(2-amino-9H-purin-9-yl)methyl]cyclopropyl}oxy)methyl]-8,8-dimethyl-3,7-dioxo-2,4,6-trioxa-3λ5-phosphanon-1-yl-pivalate maleic acid monosalt, and pharmaceutical composition containing the same.12-31-2009
20090247487Combination Therapy to Treat Hepatitis B Virus - The present invention is directed to a method for treating hepatitis B virus infection in humans comprising administering a synergistically effective amount of agents having known anti-hepatitis B virus activity in combination or alternation. Specifically, the invention is directed to a method for treating hepatitis B virus infection comprising administering FTC in combination or alternation with penciclovir, famciclovir or Bis-POM-PMEA. Additionally, the invention is directed to a method for treating hepatitis B virus infection comprising administering L-FMAU in combination or alternation with DAPD, penciclovir or Bis-POM-PMEA. The invention is further directed to a method for treating hepatitis B virus infection comprising administering DAPD in combination or alternation with Bis-POM-PMEA.10-01-2009
20110224172Substituted 1-Oxa-2,8-Diaza-Spiro [4,5] Dec-2-Ene Derivatives and Related Treatment Methods - Substituted 1-oxa-2,8-diaza-spiro[4,5]dec-2-ene compounds and processes for their production, the use thereof for producing pharmaceutical compositions, pharmaceutical compositions containing these compounds and methods of treatment using these compounds.09-15-2011
20120142635OXAZOLIDINONE-QUINOLONE HYBRID ANTIBIOTICS - The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:06-07-2012
20090203646USE OF SODIUM NARCISTATIN FOR REDUCING INTERNAL ADHESIONS AND FIBROSIS - The present invention concerns a method for reducing or preventing development of adhesions, fibrosis or scar tissue within serous body cavities by using sodium narcistatin.08-13-2009
20120077781FLAVIN DERIVATIVES - The present invention relates novel flavin derivatives and other flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives. The invention also provides method of making novel flavin derivatives.03-29-2012
20110144059PRODRUGS OF 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES - The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.06-16-2011
20090275536Antibacterial Agents - Described herein are antibacterial compounds, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical composition.11-05-2009
20090291922ANTI-PROLIFERATIVE COMPOUNDS, COMPOSITIONS, AND METHODS OF USE THEREOF - Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV,11-26-2009
20090048214Methods for Treating Renal Tumors Using 2, 4-Pyrimidinediamine Drug and Prodrug Compounds - The present disclosure provides methods for the inhibiting proliferation of tumor cells, and methods for treating solid tumor cancers in a subject by administration of 2,4-pyrimidinediamine compounds.02-19-2009
20110059921Oligomer-Nitrogenous Base Conjugates - The invention relates to (among other things) oligomer-nitrogenous base conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over unconjugated nitrogenous base compounds.03-10-2011
20100222302Novel Antibacterial Compounds - The invention relates to novel chimeric antibiotics of formula I09-02-2010
20100240613PYRIMIDINE COMPOUND AND MEDICAL USE THEREOF - The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I]09-23-2010
20120129811TRICYCLIC INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION - This invention relates to tricycle I and its therapeutic and prophylactic uses, wherein the variables C05-24-2012
20100210598TOLL-LIKE RECEPTOR MODULATORS AND TREATMENT OF DISEASES - Provided herein are small molecule conjugates that are agonists or antagonists of one or more toll-like receptors.08-19-2010
20100210599PRODRUGS OF PIPERAZINE AND SUBSTITUTED PIPERIDINE ANTIVIRAL AGENTS - This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection.08-19-2010
20100137253THERAPEUTIC COMPOUND AND TREATMENTS - Compositions and uses associated with the MT477 family of compounds are disclosed. Particular structural features and properties of the compounds are described in detail. Uses include administering an MT477 family member to a patient for therapeutic purposes. Compositions include chemicals belonging to the MT477 family and pharmaceuticals that contain such chemicals.06-03-2010
20100120717KINASE INHIBITORS - Compounds are provided for use with kinases that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture in comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.05-13-2010
20100222303REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.09-02-2010
20090111774PMEA LIPID CONJUGATES - The present invention relates to PMEA lipid conjugates and to methods of using the conjugates to treat diseases caused by viruses such as herpes, cytomegalovirus, varicella, paramyxovirus, polyoma virus, and human papillomavirus. Methods for making the PMEA lipid conjugates are also provided.04-30-2009
20110130364PYRROLOPYRIDINE DERIVATIVES SUBSTITUTED WITH CYCLIC AMINO GROUP - An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.06-02-2011
201100093672-PHENYL SUBSTITUTED IMIDAZOTRIAZINONES AS PHOSPHODIESTERASE INHIBITORS - The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.01-13-2011
20110009368SOLID FORMS OF TENOFOVIR DISOPROXIL - The Present Invention Provides Tenofovir Disoproxil Succinate, Tenofovir Disoproxil L-Tartrate, Tenofovir Disoproxil oxalate, Tenofovir disoproxil saccharate, Tenofovir disoproxil citrate, Tenofovir disoproxil salicylate and various solid forms thereof, methods for the preparation thereof and their use in pharmaceutical applications, in particular in anti-HIV medicaments. The forms of Tenofovir disoproxil can be used in combination with other anti-HIV medicaments such as Efavirenz and Emtricitabine.01-13-2011
20100179108Synthesis of Sodium Narcistatin and Related Compounds - The present invention involves use of the compounds narciclasine (2a) and 7-deoxy-narciclasine (2c), which are obtained via isolation from the medicinal plant species 07-15-2010
201301503292,4-Pyrimidinediamine Compounds and Prodrugs and Their Uses - The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I)-(III):06-13-2013
20110039803SOLID FORMS OF AN ANTI-HIV PHOSPHOINDOLE COMPOUND - Solid forms comprising a compound useful in the treatment, prevention and management of various conditions and diseases are provided herein. In particular, provided herein are solid forms comprising (2-carbamoyl-5-chloro-1H-indol-3-yl)-[3-((E)-2-cyano-vinyl)-5-methyl-phenyl]-(R)-phosphinic acid methyl ester, including salts thereof, having utility for the treatment, prevention and management of conditions and disorders including, but not limited to, human immunodeficiency virus infection.02-17-2011
20100286094NOVEL COMPOUNDS OF REVERSE TURN MIMETICS AND THE USE THEREOF - Conformationally constrained compounds that are novel and mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins and having bicyclic framework are disclosed, as well as their prodrugs. Such reverse-turn mimetic structures and pro-drugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. The invention also relates to a use of such compounds for the preparation of a medicament for treating or preventing cancer including an acute myeloid leukemia.11-11-2010
20110212924COMPOSITIONS AND METHODS TO TREAT CARDIAC DISEASES - Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)-methanocarba (bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C—P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded.09-01-2011
20090215726Phosphono-Pent-2-en-1-yl Nucleosides and Analogs - Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are 5-phosphono-pent-2-en-1-yl nucleosides and esters thereof.08-27-2009
20110082111POLO-LIKE KINASE INHIBITORS - Compounds of the following formula are provided for use with kinases:04-07-2011
20110077222Sustained-Release Opiate and Opiate Derivative Compositions - The present invention provides sustained-release opiate compositions. In particular, the present invention provides sustained-release opiate compositions that include an opiate attached to a blood albumin binder. The present invention also relates to methods of administering an opiate with a sustained release pharmacokinetic profile.03-31-2011
20110152219USE OF ENHANCERS, POSSIBLY ASSOCIATED TO RIBOFLAVIN, AS WELL AS CORRESPONDING OPHTHALMIC COMPOSITIONS FOR CORNEAL CROSS-LINKING IN THE TREATMENT OF THE KERATOCONUS OR OF OTHER CORNEAL ECTASIC DISORDERS - The use of enhancers with possibly riboflavin, as well as the corresponding compositions for the treatment of keratoconus or other ectasic corneal disorders by the method of corneal cross-linking.06-23-2011
20090258840METHOD AND COMPOSITIONS FOR TREATING HEMATOLOGICAL MALIGNANCIES - A compound of formula (1), and/or its salts, tautomers or solvates is used to treat hematological malignancies. In an embodiment, an organic acid salt of compound 1 is provided for general use in treatment of neoplasms, and in a further embodiment the salt is stabilized with carbohydrate.10-15-2009
20090253654CHOLINERGIC ENHANCERS WITH IMPROVED BLOOD-BRAIN BARRIER PERMEABILITY FOR THE TREATMENT OF DISEASES ACCOMPANIED BY COGNITIVE IMPAIRMENT - The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugs”, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.10-08-2009
20080287396Phosphonated Fluoroquinolones, Antibacterial Analogs Thereof, and Methods for the Prevention and Treatment of Bone and Joint Infections - The present invention relates to phosphonated fluoroquinolones, antibacterial analogs thereof, and methods of using such compounds. These compounds are useful as antibiotics for prevention and/or the treatment of bone and joint infections, especially for the prevention and/or treatment of osteomyelitis.11-20-2008
20080214503Hiv Integrase Inhibitors - The present intention features compounds that are HIV integrase inhibitors and may be useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.09-04-2008
20110021464METHODS OF TREATING VIRAL INFECTIONS - The present invention provides methods of treating human immunodeficiency virus (HIV) and/or hepatitis B virus (HBV) infection, including administering a compound described in the invention in an amount effective treat the HIV and/or HBV infection and at least substantially inhibit the development of resistance to said antiviral compounds in the subject. Pharmaceutical compositions are also provided.01-27-2011
20110053893COMPOUNDS AND COMPOSITIONS AS TLR ACTIVITY MODULATORS - The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 7. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.03-03-2011
20110053892Imidazo[4,5-d]Pyridazine Compounds For Treating Viral Infections - Disclosed are compounds and compositions of Formula (I), pharmaceutically acceptable salts and solvates thereof, and their preparation and uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses:03-03-2011
20100298269PRODRUGS OF CGRP RECEPTOR ANTAGONISTS - Disclosed are prodrug compounds of formula (I) (wherein variables R11-25-2010
20110136764AMINO PYRIMIDINE ANTICANCER COMPOUNDS - Compounds of Formula 1, as shown below and defined herein:06-09-2011
20110136766AURORA KINASE INHIBITORS - Disclosed herein are Aurora kinase Inhibitors represented by Structural Formula (I): Values for the variables in Structural Formula (I) are defined herein.06-09-2011
20110136765Pyrrolo[2,3-D]Pyrimidine Compounds - Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.06-09-2011
20100168064NOVEL HYDROPHILIC DERIVATIVES OF 2-ARYL-4-QUINOLONES AS ANTICANCER AGENTS - 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120 (Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and Λ/, Λ/-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.07-01-2010
20090176743Methods for treating or preventing reactivation of a latent herpesvirus infection - The invention is directed to methods and compositions for treating or preventing reactivation of a latent herpesvirus infection and the associated complications and outcomes. The methods involve administering a composition comprising glutamine, or a derivative, conjugate, or analog thereof.07-09-2009
20090176742METHODS RELATING TO THE TREATMENT OF FIBROTIC DISORDERS - The invention provides α-mimetic structure of formula (I), wherein A is —(C═O)—(CHR07-09-2009
20110263535TYROSINE-BASED PRODRUGS OF ANTIVIRAL AGENTS - A tyrosine-based (phosphonylmethoxyalkyl)purine or -pyrimidine conjugate is provided. In some embodiments, the conjugate includes tyrosine based amino acid or dipeptide moieties of (S)-9-(3-hydroxy-2-phosphonyl-methoxypropyl)adenine or its cytosine analogue. A method of synthesizing such conjugates based on Boc-protected amino acid or dipeptides is also provided. In addition, a method of isomerizing an (S,S)-diastereoisomer to an (S,R)-diastereoisomer of an amino acid-based or dipeptide-based conjugate by a process including transesterification is provided. A method of inhibiting viral infection and a method of treating viral infection based on (phosphonylmethoxyalkyl)purine or -pyrimidine conjugates is also provided.10-27-2011
20090036408COMPOSITIONS AND METHODS FOR COMBINATION ANTIVIRAL THERAPY - The present invention relates to therapeutic combinations of [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread®) and (2R,5S, cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva™, (−)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.02-05-2009
20090270352Tenofovir Disoproxil Hemi-Fumaric Acid Co-Crystal - The present invention provides a novel crystalline form of Tenofovir disoproxil fumarate (Tenofovir DF), designated Co-crystal TDFA 2:1, methods for the preparation thereof and its use in pharmaceutical applications, in particular in anti-HIV medicaments. The crystalline form TDFA 2:1 can be used in combination with other anti-HIV medicaments such as Efavirenz, Emtricitabine, Ritonavir and/or TMC114.10-29-2009
20090312288KINASE INHIBITORS - Compounds are provided for use with kinases that comprise a compound selected from the group consisting of:12-17-2009
20100210596USE OF AMINOPYRIMIDINE COMPOUNDS IN THE TREATMENT OF IMMUNE DISORDERS - The present invention provides methods of treating immune disorders. The present invention provides methods of treating an autoimmune disorder; methods of reducing the risk of transplant rejection; methods of increasing transplant survival; and methods of treating graft-versus host disease. The methods generally involve administering to an individual in need thereof an effective amount of an aminopyrimidine compound.08-19-2010
20110112052SPIRO-OXINDOLE MDM2 ANTAGONISTS - Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.05-12-2011
20110071115PHARMACEUTICALLY USEFUL HETEROCYCLE-SUBSTITUTED LACTAMS - The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, infections, and certain immunological disorders.03-24-2011
20120046246METHODS FOR TREATING OSTEOCLAST-RELATED DISEASE, COMPOUNDS AND COMPOSITIONS THEREOF - This invention relates to therapeutic methods for treating or preventing an osteoclast-related disease or disorder in a subject identified as in need of a treatment of bone diseases, compounds for such uses, and compositions thereof.02-23-2012
20120010171Nucleotide Analogue Prodrug and the Preparation Thereof - The present invention provides: 1) Derivative solid form of 9-[2-(R)-[bis[pivaloyloxymethoxy]-phosphinylmethoxy]propyl]adenine (bis-POM PMPA, abbreviated as TD hereinafter), including crystalline form A and form B of TD, TD fumarate salts and cyclodextrin inclusion complex of TD; 2) Synthesis and purification methods of TD and Solidification method of TD oil, including converting TD oil to crystalline TD in Form A and Form B, solid TD salts and cyclodextrin inclusion complex of TD; 3) Stable pharmaceutical compositions containing TD derivatives and their preparation; 4) The use of the above TD derivatives in the antiviral treatments, especially in the treatment of HIV, HBV, CMV, HSV-1, HSV-2 and human Herpes virus infections.01-12-2012
20120010170"Methods of Reducing Nephrotoxicity in Subjects Administered Nucleoside Phosphonates" - A conjugate compound comprising an acyclic nucleoside phosphonate covalently coupled to a lipid for the therapeutic and/or prophylactic treatment of viral infection in an immunodeficient subject is described, along with compositions and methods of using the same. A preferred conugate compound is CMX001, having formula (I) or a pharmaceutically acceptable salt thereof.01-12-2012
20120015907Furopyridine compounds and uses thereof - The present invention provides a compound of formula I;01-19-2012
20120015908SYNTHESIS AND ANTICANCER ACTIVITY OF ARYL AND HETEROARYL-QUINOLIN DERIVATIVES - A compound of Formula I is disclosed as follows:01-19-2012
20120058975Phosphonate Compounds - The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.03-08-2012
20120108547INHIBITORS OF TYROSINE KINASES AND USES THEREOF - Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.05-03-2012
20110092459ALPHA HELIX MIMETICS AND METHODS RELATING THERETO - Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.04-21-2011
20110092458Use of (R)-Penciclovir Triphosphate for the Manufacture of a Medicament for the Treatment of Viral Diseases - A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of such treatment, an effective amount of the (R)-enantiomer of the triphosphate of a compound of formula (A) or a pharmaceutically acceptable salt thereof; and compounds for use in the method.04-21-2011
20110092457NOVEL PHOSPHONIC ACID COMPOUNDS AS INHIBITORS OF SERINE PROTEASES - The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.04-21-2011
20110092456Methods of increasing cAMP levels and uses thereof - The present invention shows that cilostazol, a phosphodiesterase 3 inhibitor has additional beneficial effects to atorvastatin on myocardial remodeling by inducing and preserving eNOS phosphorylation. The present invention demonstrates a cardioprotective effect of Cilostazol indicating the therapeutic potency of this drug. In addition, the present invention demonstrates that the additional effect of Cilostazol and atorvastatin therapy against ischemia injury is due to the augmentation of phosphatodylicositol 3-kinase/AKT (PI3-/AKT), PKA and p-eNOS signaling.04-21-2011
20120252761KINASE INHIBITORS - Compounds are provided for use with kinases that comprise a compound selected from the group consisting of:10-04-2012
201201574112-AMINO-4-ARYLTHIAZOLE COMPOUNDS AS TRPAI ANTAGONISTS - The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.06-21-2012
201101054342-AMINO PURINE DERIVATIVES AND THEIR USE AS ANTI-HERPETIC AGENTS - Anti-herpetic material such as 2-amino purine derivatives to prevent or treat autoimmune disease or a disease originating from an abnormal functioning of the sympathetic chain in a human subject. The disease is often of a tissue or organ associated with decreased blood flow to the tissue or organ (correlated with hypertonicity of the vessels feeding the tissue or organ). The treatment reduces inflammation, scarring, destruction, and pain in the tissue or organ affected and returns the tissue or organ to nearly normal functioning, while showing none of the side effects of previous treatments. Prolonged use of the anti-herpetic compounds reduces prodrome, vesicle formation and viral shedding. The anti-herpetic compounds may be administered alone or in combination with a compound that reduces the rate of renal excretion of the anti-herpetic compound. The anti-herpetic compounds are particularly useful when administered at a level equivalent in activity to 250 mg/kg famciclovir per day.05-05-2011
20120122818LUNG-TARGETED DRUGS - Methods and compositions are provided for treating lung diseases, including but not limited to infections and small cell and non-small cell lung cancer, by conjugating a drug of interest to glycerol ethers or glycerol phosphate ethers.05-17-2012
20120316135Compounds for Inhibiting Cell Proliferation in EGFR-Driven Cancers - The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I:12-13-2012
20120316136TREATMENT OF RESPIRATORY DISORDERS USING TRPA1 ANTAGONISTS - The present patent application relates to treatment of a respiratory disorder using TRPA1 antagonists. Particularly, the present patent application relates to treatment of a respiratory disorder using a TRPA1 antagonist, wherein the TRPA1 antagonist is administered by inhalation route to a subject in need thereof.12-13-2012
20120316137Methods and Compositions for Treating Cancer - The invention features methods, kits, and pharmaceutical compositions for treating cancer using 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)-methyl)-3-(trifluoromethyl)phenyl)benzamide.12-13-2012
20120122819GUANINE RIBOSWITCH BINDING COMPOUNDS AND THEIR USE AS ANTIBIOTICS - The present invention includes novel compounds and pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against microorganisms bearing a guanine riboswitch that controls the expression of the guaA gene, including organisms which are resistant to certain antibiotic families, and which are useful as antibacterial agents for treatment or prophylaxis of bacterial infections in animals or in humans, in particular but not limited to infections of the mammary gland, or their use as antiseptics, agents for sterilization or disinfection.05-17-2012
20120122817HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF - Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.05-17-2012
20120214768NOVEL PYRIDOPYRAZINE DERIVATIVES, PROCESS OF MANUFACTURING AND USES THEREOF - The invention relates to pyrido[2,3-b]pyrazine compounds of general formulae (Ia) and (Ib), to their preparation and use, for example, for the treatment of malignant disorders and other disorders based on pathological cell proliferations.08-23-2012
20120135962COMPOSITIONS TO COMBAT ECTOPARASITES - The present invention provides a method of pesticidal treatment of vertebrate aquatic animals, in particular fish. The method includes applying to said aquatic animals, typically topically or, more preferably, by administration into water in which said aquatic animals are contained, a topical pesticidal composition comprising a pyrethroid and an organophosphate biocide in a weight ratio of 1:20 to 10:1, particularly 1:10 to 5:1, especially 1:3 to 3:1.05-31-2012
20120135963LIPIDATED OXOADENINE DERIVATIVES - Provided are novel lipidated oxoadenines which are useful as immunostimulators and adjuvants and are shown to be inducers of interferon-a and other immunostimulatory cytokines.05-31-2012
20120135961USE OF OXAZOLIDINONE-QUINOLINE HYBRID ANTIBIOTICS FOR THE TREATMENT OF ANTHRAX AND OTHER INFECTIONS - The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.05-31-2012
20120178716Unsaturated Heterocyclic Derivatives - This invention relates to compounds of the general formula:07-12-2012
20100292188Compounds Comprising A Cyclobutoxy Group - The present invention relates to compounds of formula (I) comprising a cyclobutoxy group, processes for preparing them, pharmaceutical compositions comprising said compounds and their use as pharmaceuticals.11-18-2010
20120083470INHIBITORS OF TYROSINE KINASES AND USES THEREOF - Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.04-05-2012
201101245992,4-Pyrimidinediamine Compounds and Prodrugs and Their Uses - The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I)-(III):05-26-2011
20120232036Prodrugs of 2,4-Pyrimidinediamine Compounds and Their Uses - The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.09-13-2012
20100204182ECTONUCLEOTIDASE INHIBITORS - The present invention provides ectonucleotidase inhibitors represented by the following formula, including ecto-nucleotide triphosphate diphosphohydrolase (NTPDase) inhibitors and ecto-5′-nucleotidase (ecto-5′-NT) inhibitors, namely nucleotide mimetics as selective NTPDase or ecto-5′-NT inhibitors. It also provides methods for preparations of said compounds. Furthermore provided are pharmaceutical and diagnostic compositions comprising said compounds, and the use of said compounds in a medicament for treating diseases associated with ectonucleotidase activity and/or P1 or P2 receptors.08-12-2010
20120329759FORMULATIONS AND METHODS FOR VASCULAR PERMEABILITY-RELATED DISEASES OR CONDITIONS - Described herein are formulations and methods for treating, inhibiting, preventing, delaying onset, or causing regression of a disease or condition relating to vascular permeability.12-27-2012
20120322764Acyclic Nucleoside Phosphonate Derivatives and Medical Uses Thereof - The present invention relates to an acyclic nucleoside phosphonate derivative and medical uses thereof. Specifically, the present invention relates to an acyclic nucleoside phosphonate derivative of Formula I having strong potency against viruses, such as hepatitis B virus, and low cytotoxicity, or a pharmaceutically acceptable salt, isomer, hydrate or solvate thereof, wherein R12-20-2012
20120322765PLANT DISEASE CONTROLLING COMPOSITION AND METHOD FOR CONTROLLING PLANT DISEASE - The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more inorganic fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease. group (A): a group consisting of fludioxonil, pencycuron, ametoctradin, chloroneb, chlorothalonil, oxine-copper, cyflufenamid, dichlofluanid, dicloran, diethofencarb, dinocap, dithianon, edifenphos, fenaminosulf, fentin, fluazinam, fluoroimide, flusulfamide, flutianil, fosetyl-Al, hydrargaphen, iprobenfos, metrafenon, milneb, penflufen, phosdiphen, phthalide, prothiocarb, pyrazophos, sedaxane, silthiofam, spiroxamine, tebufloquin, and tolyfluanid.12-20-2012
20120322766USE OF OXAZOLIDINONE-QUINOLINE HYBRID ANTIBIOTICS FOR THE TREATMENT OF ANTHRAX AND OTHER INFECTIONS - The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.12-20-2012
20120270842Inhibitors of Diacylglycerol O-Acyltransferase 1 (DGAT-1) and Uses Thereof - The invention pertains to use of DGAT-1 inhibitors to treat and/or prevent overweight, obesity and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease. Compounds and compositions suitable for use in the disclosed methods are also provided.10-25-2012
201102375505-AZAINDOLE BISPHOSPHONATES - Novel 5-azaindole bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.09-29-2011
20110237549MODULATORS OF RNA RIBOSWITCHES - Provided is a computer model generated from a data array, computer readable storage media encoded with the model, and computers comprising the model, wherein the model is derived from atomic structure coordinates of a FMN riboswitch or a lysine riboswitch. Further provided is a pharmacophore having a spatial arrangement of atoms defined by the binding pocket identified in the model, along with a compound defined by the pharmacophore. Also further provided are methods for rational drug design based on the atomic structure data, and compounds identified by the rational drug design process.09-29-2011
20100216746CHEMICAL COMPOUNDS - The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.08-26-2010
20120101064IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES - The invention provides compounds of the formula (I):04-26-2012
20120101065INHIBITORS OF TYROSINE KINASES AND USES THEREOF - Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.04-26-2012
20130018018NOVEL NUCLEOSIDE PHOSPHONATES AND ANALOGS - Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are nucleoside phosphonates and esters thereof.01-17-2013
20090088407COMPOUNDS, METHODS AND PHARMACEUTICAL COMPOSITIONS FOR INHIBITING PARP - The present invention provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.04-02-2009
20100173870Phosphonate Compounds - The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.07-08-2010
20110160162PRODRUGS OF A2B ADENOSINE RECEPTOR ANTAGONISTS - Disclosed are prodrugs of A06-30-2011
20130023496Combination Therapy Comprising A CCR5 Antagonist, A HIV-1 Protease Inhibtior and a Pharmacokinetic Enhancer - The present invention discloses a novel combination therapy for HIV-1 treatment relying on a combination of at least one CCR5 antagonist, at least one HIV-1 protease inhibitor and at least one pharmacokinetic enhancer of said at least one CCR5 antagonist and/or at least one HIV-1 protease inhibitor. The combination is intended for use in oral treatment of a disorder selected from the group consisting of HIV-1 infection, retroviral infections genetically related to HIV and AIDS, in a treatment-naïve patient infected with CCR5 tropic HIV-1 virus.01-24-2013
20080234231Hiv Integrase Inhibitors - The present invention features compounds that are HIV integrase inhibitors and may be useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.09-25-2008
20080227754PRODRUGS OF PHOSPHONATE NUCLEOTIDE ANALOGUES - A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a)09-18-2008
20110263534PHOSPHONATED RIFAMYCINS AND USES THEREOF FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS - The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.10-27-2011
20130116213NOVEL FUSED PYRIMIDINE DERIVATIVES FOR INHIBITION OF TYROSINE KINASE ACTIVITY - The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.05-09-2013
20130096088Inhibitors of Protein Tyrosine Kinase Activity - The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling.04-18-2013
20090118233Heterocyclic compounds having inhibitory activity against HIV integrase - A heterocyclic compound of the formula (I):05-07-2009
20090275535ANTIVIRAL PHOSPHONATE ANALOGS - The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.11-05-2009
20080200435Combinations Of A Pyrimidine Containing Nnrti With Rt Inhibitors - The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and/or nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.08-21-2008
20130137659ANTICANCER DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - Provided herein are compounds of formula (I):05-30-2013
20100317623HCV NS3 Protease Inhibitors - The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.12-16-2010
20130184240HETERO RING-FUSED IMIDAZOLE DERIVATIVE HAVING AMPK ACTIVATING EFFECT - Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula:07-18-2013
20120283220ANTOFINE AND CRYPTOPLEURINE DERIVATIVES AS ANTICANCER AGENTS - The present invention provides compounds of Formula (I-IV): compositions containing the same, and methods of use thereof such as for the treatment of cancer.11-08-2012
20120283219DIAMINOPTERIDINE DERIVATIVES - The present invention relates novel diaminopteridine derivatives, their compositions and method of treatment comprising the same for use as anti-infectives.11-08-2012
20090143335MODIFIED ABSORPTION FORMULATION OF GABOXADOL - The present invention relates to a pharmaceutical composition comprising gaboxadol or a pharmaceutically acceptable salt thereof and one or more inhibitors of PAT1 and/or one or more inhibitors of OAT. The present invention further relates to a pharmaceutical composition comprising from about 0.5 mg to about 50 mg gaboxadol or a pharmaceutically acceptable salt thereof, wherein the composition provides an in vivo plasma profile comprising a mean Tmax which is longer than about 20 minutes.06-04-2009
20080318904DEUTERIUM-ENRICHED TENOFOVIR - The present application describes deuterium-enriched tenofovir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.12-25-2008
20090318387ALKYNYL PYRROLO[2,3-d]PYRIMIDINES AND RELATED ANALOGS AS HSP90-INHIBITORS - Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of various HSP90 mediated disorders. Methods of synthesis and use of such compounds are also described and claimed.12-24-2009
20120028925APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.02-02-2012
20130210771METHODS AND COMPOSITIONS FOR TREATING CANCERS - This invention provides a combination of antagonists of the hedgehog signaling pathway with a BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with protein tyrosine kinases such as, for example, Src, BCR-ABL and c-kit.08-15-2013

Patent applications in class Nonshared hetero atoms in at least two rings of the polycyclo ring system